Zhang Jinfeng, Li Shengliang, An Fei-Fei, Liu Juan, Jin Shubin, Zhang Jin-Chao, Wang Paul C, Zhang Xiaohong, Lee Chun-Sing, Liang Xing-Jie
Nano-organic Photoelectronic Laboratory, Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, 100190 Beijing, P. R. China.
Nanoscale. 2015 Aug 28;7(32):13503-10. doi: 10.1039/c5nr03259h. Epub 2015 Jul 22.
The use of different nanocarriers for delivering hydrophobic pharmaceutical agents to tumor sites has garnered major attention. Despite the merits of these nanocarriers, further studies are needed to improve their drug loading capacities (which are typically <10%) and reduce their potential systemic toxicity. Therefore, the development of alternative self-carried nanodrug delivery strategies without using inert carriers is highly desirable. In this study, we developed a self-carried curcumin (Cur) nanodrug for highly effective cancer therapy in vitro and in vivo with real-time monitoring of drug release. With a biocompatible C18PMH-PEG functionalization, the Cur nanoparticles (NPs) showed excellent dispersibility and outstanding stability in physiological environments with drug loading capacities >78 wt%. Both confocal microscopy and flow cytometry confirmed the cellular fluorescence "OFF-ON" activation and real-time monitoring of the Cur molecule release. In vitro and in vivo experiments clearly show that the therapeutic efficacy of the PEGylated Cur NPs is considerably better than that of free Cur. This self-carried strategy with real-time monitoring of drug release may open a new way for simultaneous cancer therapy and monitoring.
使用不同的纳米载体将疏水性药物输送到肿瘤部位已引起了广泛关注。尽管这些纳米载体有诸多优点,但仍需要进一步研究以提高其载药量(通常<10%)并降低其潜在的全身毒性。因此,开发无需使用惰性载体的替代性自载纳米药物递送策略非常必要。在本研究中,我们开发了一种自载姜黄素(Cur)纳米药物,用于在体外和体内进行高效癌症治疗,并对药物释放进行实时监测。通过生物相容性的C18PMH-PEG功能化,Cur纳米颗粒(NPs)在生理环境中表现出优异的分散性和出色的稳定性,载药量>78 wt%。共聚焦显微镜和流式细胞术均证实了细胞荧光的“关闭-开启”激活以及Cur分子释放的实时监测。体外和体内实验清楚地表明,聚乙二醇化Cur NPs的治疗效果明显优于游离Cur。这种具有药物释放实时监测功能的自载策略可能为同步癌症治疗和监测开辟一条新途径。